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LG-121071
LG121071 (or LGD-121071) is a selective androgen receptor modulator (SARM) developed by Ligand Pharmaceuticals that was first described in 1999 and was the first orally active nonsteroidal androgen to be discovered. It is a tricyclic quinolone derivative, structurally distinct from other nonsteroidal AR agonists like andarine and enobosarm (ostarine). The drug acts as a high-affinity full agonist of the androgen receptor (AR) (Ki = 17 nM), with a potency and efficacy that is said to be equivalent to that of dihydrotestosterone (DHT). Unlike testosterone, but similarly to DHT, LG121071 and other nonsteroidal androgens cannot be potentiated by 5α-reductase in androgenic tissues (nor aromatized into estrogenic metabolites), and for this reason, show tissue-selective androgenic effects. In accordance, they are said to possess full anabolic activity with reduced androgenic activity, similarly to anabolic-androgenic steroids. The ''in vitro'' metabolism Metabolism (, from ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
LG-120907
LG-120907 is a nonsteroidal antiandrogen (NSAA) of the quinoline group which was developed by Ligand Pharmaceuticals along with selective androgen receptor modulators (SARMs) like LG-121071 and was never marketed. The drug is a high-affinity antagonist of the androgen receptor (AR) with a Ki value of 26 nM and has been found to inhibit growth of the ventral prostate and seminal vesicles in male rats without increasing circulating levels of luteinizing hormone or testosterone. However, this tissue selectivity has not been assessed in humans. LG-120907 is orally active and shows greater oral potency than the aryl propionamide NSAA flutamide. The 7-fluoro derivative of LG-120907, LG-105, is also a potent NSAA, and appears to possess greater potency in comparison. Conversely, the 6- ethyl, 8-di desmethyl analogue of LG-120907, LG-121071, is a SARM with potent androgenic activity equivalent to that of dihydrotestosterone Dihydrotestosterone (DHT, 5α-dihydrotestoster ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Selective Androgen Receptor Modulator
Selective Androgen Receptor Modulators or SARMs are a class of androgen receptor ligands that maintain some of the desirable effects of androgens, such as preventing osteoporosis and muscle loss while reducing risks of developing prostate cancer. In the late 1990s, the first nonsteroidal SARM, an analog of bicalutamide, was discovered. They are intended to have the same kind of effects as androgenic drugs, such as anabolic-androgenic steroids, but be more selective in their action. At present, there are no SARMs which have been approved for therapeutic use by the U.S. Food and Drug Administration. Comparison to testosterone As previously mentioned, the purpose of research in relation to SARMs is to replace testosterone supplementation in disease treatment with selective androgen receptor molecules. This is due to the fact that testosterone supplementation can have adverse effects on patients, which are detailed on the testosterone page. Thinking of testosterone as a model m ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Acetothiolutamide
Acetothiolutamide is a selective androgen receptor modulator (SARM) derived from the nonsteroidal antiandrogen bicalutamide that was described in 2002 and was one of the first SARMs to be discovered and developed. It is a high-affinity, selective ligand of the androgen receptor (AR) (Ki = 2.1–4.9 nM), where it acts as a full agonist ''in vitro'', and has ''in vitro'' potency comparable to that of testosterone. However, ''in vivo'', acetothiolutamide displayed overall negligible androgenic effects, though significant (albeit very low) anabolic effects were observed at high doses. In addition, notable antiandrogen effects were observed in castrated male rats treated with testosterone propionate. The discrepancy between the ''in vitro'' and ''in vivo'' actions of acetothiolutamide was determined to be related to rapid plasma clearance and extensive hepatic metabolism into a variety of metabolites with differing pharmacological activity, including AR partial agonism and antagonism ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Aromatized
Aromatization is a chemical reaction in which an aromaticity, aromatic system is formed from a single nonaromatic precursor. Typically aromatization is achieved by dehydrogenation of existing cyclic compounds, illustrated by the conversion of cyclohexane into benzene. Aromatization includes the formation of heterocyclic systems. : Industrial practice Although not practiced under the name, aromatization is a cornerstone of oil refining. One of the major reforming reactions is the dehydrogenation of naphthenes into aromatics. The process, which is catalyzed by platinum, is exemplified in the conversion methylcyclohexane (a naphthene) into toluene (an aromatic). Dehydrocyclization converts paraffins (acyclic hydrocarbons) into aromatics. A related aromatization process includes dehydroisomerization of methylcyclopentane to benzene: : Biochemical processes : Aromatases are enzymes that aromatize rings within steroids. The specific conversions are testosterone to estradiol and and ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
S-40503
S-40503 is an investigational selective androgen receptor modulator (SARM) developed by the Japanese company Kaken Pharmaceuticals, which was developed for the treatment of osteoporosis. SARMs are a new class of drugs which produce tissue-specific anabolic effects in some tissues such as muscle and bone, but without stimulating androgen receptors in other tissues such as in the prostate gland, thus avoiding side effects such as benign prostatic hypertrophy which can occur following treatment with unselective androgens like testosterone or anabolic steroids. S-40503 is a SARM that shows good functional selectivity for bone tissue, and has relatively little effect on muscle mass and no observable effect on the prostate gland. In animal studies it was shown to increase both bone mineral density and biomechanical strength of femoral cortical bone, and at low doses showed anabolic effects only on bone tissue, while at higher doses both bone and muscle growth were affected, yet pros ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
LGD-3303
LGD-3303 is a drug which acts as a selective androgen receptor modulator (SARM), with good oral bioavailability. It is a selective agonist for the androgen receptor, producing functional selectivity with effective dissociation of anabolic and androgenic effects, acting as a partial agonist for androgenic effects, but a full agonist for anabolic effects. It has been investigated as a possible treatment for osteoporosis, and was shown in animal studies to enhance the effectiveness of a bisphosphonate Bisphosphonates are a class of drugs that prevent the loss of bone density, used to treat osteoporosis and similar diseases. They are the most commonly prescribed drugs used to treat osteoporosis. They are called bisphosphonates because they ... drug. References Indoles Lactams Organochlorides Organofluorides Selective androgen receptor modulators Trifluoromethyl compounds {{genito-urinary-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
LGD-2226
LGD-2226 is an investigational selective androgen receptor modulator (SARM), which is being developed for treatment of muscle wasting and osteoporosis. LGD-2226 is an orally active, potent and selective agonist for androgen receptors which was shown to have anabolic effects in both muscle and bone tissue, but with considerably less effects on prostate weight and luteinizing hormone levels than testosterone. Selective androgen receptor modulators may also be used by athletes to assist in training and increase physical stamina and fitness, potentially producing effects similar to anabolic steroids but with significantly less side effects. For this reason, SARMs have already been banned by the World Anti-Doping Agency The World Anti-Doping Agency (WADA; french: Agence mondiale antidopage, AMA) is a foundation initiated by the International Olympic Committee based in Canada to promote, coordinate, and monitor the fight against drugs in sports. The agency's key ... since Janu ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Doping Agent
A dopant, also called a doping agent, is a trace of impurity element that is introduced into a chemical material to alter its original electrical or optical properties. The amount of dopant necessary to cause changes is typically very low. When doped into crystalline substances, the dopant's atoms get incorporated into its crystal lattice. The crystalline materials are frequently either crystals of a semiconductor such as silicon and germanium for use in solid-state electronics, or transparent crystals for use in the production of various laser types; however, in some cases of the latter, noncrystalline substances such as glass can also be doped with impurities. In solid-state electronics using the proper types and amounts of dopants in semiconductors is what produces the p-type semiconductors and n-type semiconductors that are essential for making transistors and diodes. Transparent crystals Lasing media The procedure of doping tiny amounts of the metals chromium (Cr), ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Metabolism
Metabolism (, from el, μεταβολή ''metabolē'', "change") is the set of life-sustaining chemical reactions in organisms. The three main functions of metabolism are: the conversion of the energy in food to energy available to run cellular processes; the conversion of food to building blocks for proteins, lipids, nucleic acids, and some carbohydrates; and the elimination of metabolic wastes. These enzyme-catalyzed reactions allow organisms to grow and reproduce, maintain their structures, and respond to their environments. The word metabolism can also refer to the sum of all chemical reactions that occur in living organisms, including digestion and the transportation of substances into and between different cells, in which case the above described set of reactions within the cells is called intermediary (or intermediate) metabolism. Metabolic reactions may be categorized as '' catabolic'' – the ''breaking down'' of compounds (for example, of glucose to pyruvate ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
In Vitro
''In vitro'' (meaning in glass, or ''in the glass'') studies are performed with microorganisms, cells, or biological molecules outside their normal biological context. Colloquially called " test-tube experiments", these studies in biology and its subdisciplines are traditionally done in labware such as test tubes, flasks, Petri dishes, and microtiter plates. Studies conducted using components of an organism that have been isolated from their usual biological surroundings permit a more detailed or more convenient analysis than can be done with whole organisms; however, results obtained from ''in vitro'' experiments may not fully or accurately predict the effects on a whole organism. In contrast to ''in vitro'' experiments, '' in vivo'' studies are those conducted in living organisms, including humans, and whole plants. Definition ''In vitro'' ( la, in glass; often not italicized in English usage) studies are conducted using components of an organism that have been isolated ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Anabolic-androgenic Steroid
Anabolic steroids, also known more properly as anabolic–androgenic steroids (AAS), are steroidal androgens that include natural androgens like testosterone as well as synthetic androgens that are structurally related and have similar effects to testosterone. They increase protein within cells, especially in skeletal muscles, and also have varying degrees of virilizing effects, including induction of the development and maintenance of masculine secondary sexual characteristics such as the growth of facial and body hair. The word ''anabolic'', referring to anabolism, comes from the Greek ἀναβολή ''anabole'', "that which is thrown up, mound". Androgens or AAS are one of three types of sex hormone agonists, the others being estrogens like estradiol and progestogens like progesterone. AAS were synthesized in the 1930s, and are now used therapeutically in medicine to stimulate muscle growth and appetite, induce male puberty and treat chronic wasting conditions, such as canc ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
